title: Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.
abstract: A series of cinnamide derivatives was designed as potential antimycobacterial agents using molecular hybridization approach. The diamine moiety, a key feature of ethambutol and its other analogs, and certain structural features of cerulenin and cinnamic acid were hybridized to obtain cinnamide derivatives. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against M. tuberculosis H(37)R(v) using Resazurin Microtitre plate Assay (REMA) method. The synthesized molecules showed good to moderate activity with MIC in the range of 5-150 μM and good safety profile. Additionally, the most potent compound 1a, having MIC 5.1 μM exhibited synergy with rifampicin.
authors.affiliation: Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, NP Marg, Matunga, Mumbai 400 019, India.
authors.forename: Manoj D
authors.initials: MD
authors.lastname: Kakwani
authors.forename: Prashant
authors.initials: P
authors.lastname: Suryavanshi
authors.forename: Muktikant
authors.initials: M
authors.lastname: Ray
authors.forename: M G R
authors.initials: MG
authors.lastname: Rajan
authors.forename: Sharmila
authors.initials: S
authors.lastname: Majee
authors.forename: Abdul
authors.initials: A
authors.lastname: Samad
authors.forename: Padma
authors.initials: P
authors.lastname: Devarajan
authors.forename: Mariam S
authors.initials: MS
authors.lastname: Degani
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D002934:Cinnamates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects* / Q000235:genetics; D009693:Nucleic Acid Hybridization; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D002934:Cinnamates; C029010:cinnamic acid